喜樹鹼及其衍生物的歷史回顧及展望

The Historical Review of Camptothecin and Its Derivatives

楊士平(Shih-Ping Yang) ； 李慶國(Ching-Kuo Lee)

《化學》 67卷1期 (2009/03) Pp. 45-60

https://doi.org/10.6623/chem.2009004

摘要

喜樹鹼類衍生藥物如Topotecan、Irinotecan 目前已在臨床上作為抗癌藥物，而喜樹鹼本身是從天然物中所分離出來的，探究其整個發展史，可對天然物在近代的研究方式，以及開發成藥物前所需克服的難題有基本的認識。本文就喜樹鹼的發現、結構的確立、發展中的低潮期、藥理機轉的發現、構效關係、生產策略等，做一通盤的介紹。

關鍵字

喜樹鹼 ； 生物活性導引分離 ； 構效關係 ； 組織培養

並列摘要

Among the camptothecin derivatives, such as topotecan and irinotecan, many have now reached the clinic as a promising anticancer agent, and camptothecin is isolated from natural products. To study the history of development, we heed a basic understanding about the research in natural products in recent years, and the difficulties in the course of drug development. This article has been subdivided into six major sections: (1) The discovery of camptothecin. (2) Structure determination of camptothecin. (3) The low ebb of development. (4) The discovery of novel mechanisms of action. (5) Structure activity relationships of camptothecin. (6) The strategy in the production of camptothecin.

並列關鍵字

Camptothecin ； Bioactivity-directed fractionation ； Topoisomerase I ； Structure activity relationships ； Cell tissue culture